Developments in Local Anaesthetic Drugs
Highlights
- One of the specific features of bupivacaine is that clinical evidence of accumulation of the drug in plasma may be diminished until a fairly late stage because of its high affinity for plasma protein binding sites. The ‘free’ concentration of drug in plasma remains low until all the protein binding sites are fully occupied after which it increases rapidly, and toxicity can occur without patients exhibiting signs of CNS toxicity before cardiovascular collapse (View Highlight)
- bupivacaine has been shown to have selective cardiac effects related to the slow rate at which it dissociates from the sodium channel (View Highlight)
- Ropivacaine and levobupivacaine are two relatively new amide local anaesthetic agents that have been produced in order to address the issue of bupivacaine cardiotoxicity. Each is produced as a pure ‘S’ isomer (View Highlight)
- lower lipid solubility of ropivacaine results in less motor block than bupivacaine (View Highlight)